All Photos(1)
Synonym(s):
PrCP Inhibitor, Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-Amino-N-((2 S,3 S)-3-(biphenyl-4-yl)-1-((, Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-Amino-N-((2S,3S)-3-(biphenyl-4-yl)-1-((2
Empirical Formula (Hill Notation):
C31H33Cl2N5O2
Recommended Products
Assay
≥97% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 100 mg/mL
storage temp.
−20°C
General description
A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 = 1 nM against human PrCP; IC50 = 2 and 8 nM against mouse PrCP, respectively, in the absence or presence of 1% mouse serum albumin), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC50 >25 µM). Oral administration (100 mg/kg/d for 5 d) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice in vivo.
A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC50 in the absence/presence of 1% mouse serum albumin = 1 nM/1 nM and 2 nM/8 nM, respectively, against human and mouse PrCP-catalyzed Mca-APK(Dnp)-OH hydrolysis; Initial [Substrate] = 25 µM), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC50 >25 µM). Despite its being a substrate of P-gp efflux transporters and ineffective CNS delivery across blood-brain barrier, peripheral PrCP inhibition via oral administration (100 mg/kg/d for 5 d; [Drug] = 380 nM and 50 nM, respectively, in blood and brain 24 h after last p.o. dosing) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice (0.73 g fat reduction vs. 0,73 g fat gain in 5 d, respectively, with drug or vehicle treatment) in vivo. Drug treatment among PrCP-/- obsese mice in comparison, results in only 1.1% weight loss primarily due to a decreased gain in muscle mass and little change in body fat.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PrCP
PrCP
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Use only fresh DMSO for reconstitution.
Other Notes
Wu, Z., et al. 2012. Bioorg. Med. Chem. Lett.22, 1774.
Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett.22, 658.
Zhou, C., et al. 2010. J. Med. Chem.53, 7251.
Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett.22, 658.
Zhou, C., et al. 2010. J. Med. Chem.53, 7251.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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